Application method for enhanced oral assimilation through oral and gastrointestinal membranes, of liquids containing insulin, or other drugs, by enclosing them in stable, nanometer size, vesicles formed with a special combination of essential phospholipids (EPL) to minimize side effects and maximize absorption in oral applications

ABSTRACT

The intend of this invention is to produce stable, non-leaking Essential Phospholipid (EPL) nano spheres for oral administration of insulin, chelating agents, and other substances, which are able to effectively bridge the gastrointestinal barrier for systemic treatment.

BACKGROUND OF THE INVENTION

[0001] (1) Technical Field

[0002] Administration of Essential Phopholipid (EPL) Nano-encapsulatedsubstances orally for the purpose of allowing transport through the oraland gastrointestinal membranes into the human or animal vascular system.

[0003] (2) Description of the Related Art

[0004] EPL Nano Capsules, also called vesicles or liposomes, have beenused in the past to transport liquid substances through the epidermisthrough topical applications and also intravenously to deliver drugs.Applications to transport drugs orally and through the gastrointestinaltract have not been successful because the nano meter size capsules wereprematurely destroyed in the Gastro-Instestinal tract and/or leakingencapsulated substances causing severe side effects to the stomach andthe intestines. For example: about one half gram or more of Di-SodiumEDTA, given orally in an aqueous solution, cause immediate diarrheawhile only less than 5% of the administered amount crosses into theblood stream. Even if encapsulated in specific phopholipids., likephoshatidylcholin, the same effect occurs and negligible amounts of f.i.Di-Sodium EDTA pass into the blood stream. The inventor has developed aspecific combination different kinds of natural phospholipids whichallow close to 90% of the administered solution to pass into thevascular system, without side effects in the gastrointestinal tract.

BRIEF SUMMARY OF THE INVENTION

[0005] This invention relates to a novel method of creating stableEssential Phospholipid nano-spheres for enclosing insulin, or othersubstances. These micro-spheres are generated with the aid of specialcombinations of Essential Phospholipids. The property of these specialcombinations are such that the EPL micro-spheres become more stable inthe gastrointestinal tract and avoid leakage of the encapsulatedsubstance and the associated side effects.

BRIEF DESCRIPTION OF THE SEVERAL VIEWS OF THE DRAWINGS

[0006] N/A

DETAILED DESCRIPTION OF THE INVENTION

[0007] This invention relates to a novel method of creating stableEssential Phospholipid nano-spheres for encapsulating insulin and otherdrugs. These nano-spheres are generated with the aid of specialcombinations of Essential Phospholipids. The property of these specialcombinations are such that the EPL nano-spheres become more stable inthe gastrointestinal tract and avoid leakage of the encapsulatedsubstance. Since many of the encapsulated substances may cause seriousside effects in the gastrointestinal tract when taken in large doses,like insulin or Di-Sodium EDTA, and vitamin C, stability of themicro-spheres is of great importance.

[0008] As a typical example we will describe the effect of Di-SodiumEDTA on the human system and especially on the gastrointestinal tract.Di-Sodium EDTA is extensively used in detoxification of the humansystem, especially for the removal of heavy metals. Di-Sodium EDTA is avery effective chelator, i.e. it captures dangerous heavy metal ions andallows the body to discharge them harmlessly through the kidneys. Up tonow this is accomplished by dripping solutions containing 1-3 gram ofDi-Sodium EDTA per treatment into the veins of the patient requiring 30and more treatments for a single detoxifications.

[0009] When as little as 0.5 gram dose of Di-Sodium EDTA is taken orallywith water, the bowels are emptied promptly and diarrhea results. Onlyless than 5% of the ingested dose makes it into the blood stream. When 2gram or more of Di-Sodium EDTA is nano encapsulated using a single EPL,such as Phosphotidylcholin (the most abundant EPL), the samegastro-intestinal effect of diarrhea is observed, a clear indicationthat the microspheres consisting of only Phosphotidylcholine are leakingand are destroyed early in the digestive process.

[0010] However, when a special combination of EPLs is used, as developedby the inventor, to form nano-spheres, over 90% of the Di-Sodium EDTA isfound in the bloodstream and no side effects on the gastrointestinalsystem are observed. This is also the case with other substances takenin large doses, such as vitamin C (10 gram per dose). To substantiatethis claim, the inventor caused a clinical test to be performed toverify the passage of Di-Sodium EDTA from the gastrointestinal tractinto the blood stream using special combinations of EPLs. This ClinicalTest is unpublished as of this date. The results are as follows:

[0011] Clinical Absorption Study of Orally Administered Disodium EDTA on16 Patients Performed by Dr. Daniel Dugi.

[0012] The purpose of this study is to prove the safety andeffectiveness of using di-sodium EDTA orally in an essentialphospholipid (EPL) microsphere delivery system, effectively bridging theintestinal barrier, for systemic heavy metal detoxification. This novelnew oral form of di-sodium EDTA was developed by Nikolaus J. Smeh andtested clinically with sixteen patients. A baseline 24 hour urine wasinitially collected followed by provocation of two fluid ounces of aLipoflow EDTA concentrate in fruit juice, containing one gram ofdi-sodium EDTA micro encapsulated in essential phospholipids. Twosuccessive twenty-four hour urine collections followed the initialprovocation. Excellent maximum increases in urine excretion overbaseline control results were obtained: Aluminum >>100%, 960 ug/24 hr,Antimony 50%, Arsenic 1,558%, Bismuth 6,801%, Cadmium 233%, Lead 4,333%,Mercury 312%, Nickel 1,988%, Platinum >100%: 0.05 ug/24 hours, Thallium300%, Thorium >100%: 0.05 ug/24 hours, Tin 1,980%, Tungsten 150% andUranium >100%: 0.09 ug/24 hours.

1. Any natural or synthetic oral or topical delivery system using aspecial combination of Essential Phospholipids to nano encapsulateInsulin and other drugs. The new combination used to form stablemicrospheres is obtained by combining the following Phospholipids invarious proportions: (1) Phosphatidylcholine (PC) (2)Phosphatidylethanolamine (PE) (3) Phosphatidylinositol (PI) (4) MinorPhospholipids
 2. Any natural or synthetic oral delivery system using aspecial combination of Essential Phospholipids, as defined in claim 1,to nano encapsulate vitamin C from any source intended for enhanced oralassimilation for the purpose of passing these substances into thevascular system through the gastrointestinal tract.
 3. Any natural orsynthetic oral delivery system using a special combination of EssentialPhospholipids, as defined in claim 1, to micro encapsulateethylenediaminetetraacctic acid chelates intended for enhanced oralassimilation for the purpose of passing these substances into thevascular system through the gastrointestinal tract.